Page last updated: 2024-11-04

1h-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one: structure given in first source; inhibits guanylyl cyclase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one : A member of the class of oxadiazoloquinoxalines that is 1H-[1,2,4]oxadiazolo[4,3-a]quinoxaline substituted at position 1 by an oxo group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID1456
CHEMBL ID598952
CHEBI ID91215
SCHEMBL ID210817
MeSH IDM0250951

Synonyms (66)

Synonym
HMS3266N10
BRD-K26015241-001-01-0
EU-0100953
1h-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, powder
lopac-o-3636
NCGC00015770-01
tocris-0880
NCGC00024841-01
LOPAC0_000953
1h-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (9ci)
odq ,
41443-28-1
1h-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one
NCGC00024841-03
NCGC00024841-02
[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one
1h-odq
1-h-[1,2,4]oxadiazolo-[4,3,2]quinoxalin-1-ine
1h-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one
NCGC00015770-03
O 3636
NCGC00015770-05
1h-[1,2,4]oxadiazolo[4,3-a]-quinoxalin-1-one
CHEMBL598952
A7039
HMS3262P08
O0400
CCG-205034
S9796
NCGC00015770-04
NCGC00015770-02
FT-0673321
LP00953
gtpl5234
SCHEMBL210817
tox21_500953
NCGC00261638-01
CHEBI:91215
(3-methylbiphenyl-4-yl)amine
1h-(1,2,4)oxadiazolo-(4,3,a)quinoxalin-1-one
3-methyl(1,1'-biphenyl)-4-amine
S57V2NMV38 ,
(1,1'-biphenyl)-4-amine, 3-methyl-
HB2900
AC-26876
AKOS024458675
HMS3649K18
mfcd00792620
DTXSID2036796
unii-s57v2nmv38
CS-0021047
HY-101255
P16885
sr-01000075519
SR-01000075519-1
SR-01000075519-3
AS-53689
1h-[1,2,4]oxadiazole[4,3-a]quinoxalin-1-one
BCP06748
HMS3675B16
Q27088147
SR-01000075519-6
HMS3411B16
SDCCGSBI-0050927.P002
EX-A3500
NCGC00015770-10

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"The results presented in this study indicate that the toxic response brought about by increasing concentrations of tert-butylhydroperoxide in CHP100 cells was mitigated significantly by exogenously added nitric oxide donors via a cyclic GMP-independent mechanism."( Different signalling pathways mediate the opposite effects of endogenous versus exogenous nitric oxide on hydroperoxide toxicity in CHP100 neuroblastoma cells.
Cantoni, O; Clementi, E; Guidarelli, A; Sciorati, C, 1999
)
0.3
" Furthermore, while the toxic effect of NOR3 was attenuated by replacing the medium at 20 min, 1 or 2 h after drug addition, it was continued by replacing the medium at 3 h or later after drug addition."( Kinetic characterization of the nitric oxide toxicity for PC12 cells: effect of half-life time of NO release.
Kato, T; Nakamura, K; Yamamoto, H; Yamamoto, T; Yuyama, K, 2000
)
0.31

Pharmacokinetics

ExcerptReferenceRelevance
" This pharmacodynamic phenomenon is referred to in the present work as "teleantagonism"."( Teleantagonism: A pharmacodynamic property of the primary nociceptive neuron.
Cunha, FQ; Duarte, DB; Ferrari, LF; Ferreira, SH; Funez, MI; Lorenzetti, BB; Parada, CA; Sachs, D, 2008
)
0.35

Bioavailability

ExcerptReferenceRelevance
"N-acetyl-L-cysteine exerts direct anti-aggregating effects through an increased bioavailability of platelet nitric oxide."( N-acetyl-L-cysteine exerts direct anti-aggregating effect on human platelets.
Anfossi, G; Cavalot, F; Massucco, P; Mattiello, L; Russo, I; Trovati, M, 2001
)
0.31
" High glucose inhibits nitric oxide (NO) bioavailability and decreased NO increases TGF-beta activity and extracellular matrix accumulation."( Nitric oxide and cGMP-dependent protein kinase regulation of glucose-mediated thrombospondin 1-dependent transforming growth factor-beta activation in mesangial cells.
Darley-Usmar, V; Murphy-Ullrich, JE; Poczatek, MH; Shiva, S; Wang, S, 2002
)
0.31
"Acute respiratory distress syndrome (ARDS) is associated with increased superoxide (O(2)(*-)) formation in the pulmonary vasculature and negation of the bioavailability of nitric oxide (NO)."( Sildenafil citrate and sildenafil nitrate (NCX 911) are potent inhibitors of superoxide formation and gp91phox expression in porcine pulmonary artery endothelial cells.
Angelini, GD; Jeremy, JY; Muzaffar, S; Shukla, N; Srivastava, A, 2005
)
0.33
" Nonetheless, DM may cause uncoupling of nitric oxide synthases (NOSs) with reduction in the bioavailability of nitric oxide (NO), which is critical to maintain oocyte viability and prevent aging."( Activation of the cGMP signaling pathway is essential in delaying oocyte aging in diabetes mellitus.
Abu-Soud, HM; Diamond, MP; Gonik, B; Goud, AP; Goud, PT, 2006
)
0.33
" This study provides the first evidence that increased denitrosylation leads to increased bioavailability of NO, independent of NOS activity, to promote sustained angiogenesis."( The release of nitric oxide from S-nitrosothiols promotes angiogenesis.
Ahmad, S; Ahmed, A; Ahmed, S; Al-Ani, B; Cudmore, M; Fujisawa, T; Hewett, PW, 2006
)
0.33
" Since nitric oxide bioavailability is decreased in sickle cell disease and nitric oxide may inhibit leukocyte adhesion, we investigated whether stimulation of NO-signaling pathways can reduce the adhesive properties of neutrophils from sickle cell disease individuals (sickle cell diseaseneu)."( Increased adhesive properties of neutrophils in sickle cell disease may be reversed by pharmacological nitric oxide donation.
Canalli, AA; Conran, N; Costa, FF; Franco-Penteado, CF; Saad, ST, 2008
)
0.35
" The present study demonstrated that iNOS-derived superoxide generation was reduced, and that the NO bioavailability was increased, by treatment with the NOS-cofactor, tetrahydrobiopterin (BH4), before I/R in the hearts isolated from diabetic rats."( Reversal of inducible nitric oxide synthase uncoupling unmasks tolerance to ischemia/reperfusion injury in the diabetic rat heart.
Fujita, M; Ito, S; Iwasaka, T; Katano, T; Okazaki, T; Otani, H; Shimazu, T; Yoshioka, K, 2011
)
0.37
" These results suggest that BAY 60-2770 would be effective in the treatment of erectile dysfunction when NO bioavailability is reduced, after pelvic nerve injury, and when sGC is oxidized."( The sGC activator BAY 60-2770 has potent erectile activity in the rat.
Frink, TJ; Kadowitz, PJ; Lasker, GF; Pankey, EA; Walter, KA; Zeitzer, JR, 2013
)
0.39

Dosage Studied

ExcerptRelevanceReference
" In thoracic aortic rings from CH rats, cumulative dose-response curves to phenylephrine (PE) in the presence of the nitric oxide (NO) synthase inhibitor Nomega-nitro-L-arginine (L-NNA) and the HO inhibitor zinc protoporphyrin 9 (ZnPPIX) elicited increased contractility compared with CH rings treated with only L-NNA."( Role of endothelial carbon monoxide in attenuated vasoreactivity following chronic hypoxia.
Caudill, TK; Kanagy, NL; Resta, TC; Walker, BR, 1998
)
0.3
" Dose-response curves were determined with N(G)-nitro-L-arginine (L-NNA) a competitive inhibitor of nitric oxide (NO) synthase; 1H-¿1,2,4ŏxadiazolol¿4, 3aquinoxalin-1-one (ODQ), an inhibitor of soluble guanylate cyclase; and oxyhemoglobin, a scavenger of nitric oxide."( Characterization of the off response to electrical field stimulation in gallbladder smooth muscle.
Conklin, JL; Cullen, JJ; Hinkhouse, MM, 2000
)
0.31
" At high (>300 mmHg) vs low (<55 mmHg) oxygen tension the dose-response curves to NO- and SNP-induced relaxations were biphasic and shifted leftward."( Nitric oxide and sodium nitroprusside-induced relaxation of the human umbilical artery.
Lovren, F; Triggle, C, 2000
)
0.31
" Dose-response curves (10(-9) to 10(-6) M) to 5,6-EET, 8,9-EET, 11,12-EET, 14,15-EET, and ACh (10(-9) to 10(-4) M) were evaluated in preconstricted (10(-6) mol/l phenylephrine) mesenteric arteries (<350 microm diameter) in the presence or absence of 1) the cyclooxygenase inhibitor indomethacin (2."( Rat mesenteric arterial dilator response to 11,12-epoxyeicosatrienoic acid is mediated by activating heme oxygenase.
Abraham, NG; Bolognesi, M; Di Pascoli, M; Gatta, A; McGiff, JC; Sacerdoti, D; Schwartzman, ML, 2006
)
0.33
" In each case, the dose-response curve for N(2)O was progressively shifted to the right by increasing the dose of each pretreatment drug."( Involvement of a NO-cyclic GMP-PKG signaling pathway in nitrous oxide-induced antinociception in mice.
Chung, E; Ohgami, Y; Quock, LP; Quock, RM; Zhang, Y, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
EC 4.6.1.2 (guanylate cyclase) inhibitorAn EC 4.6.* (P-O lyase) inhibitor that interferes with the action of enzyme guanylate cyclase (EC 4.6.1.2).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
oxadiazoloquinoxalineAn organic heterotricyclic compound that consists of an oxadiazole ring ortho-fused at any position to a quinoxaline ring system.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (49)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID1705
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency2.78300.004023.8416100.0000AID485290
Chain A, HADH2 proteinHomo sapiens (human)Potency25.56480.025120.237639.8107AID886; AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency25.56480.025120.237639.8107AID886; AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.18380.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency39.81075.623417.292931.6228AID2323
thioredoxin reductaseRattus norvegicus (Norway rat)Potency26.40760.100020.879379.4328AID488772; AID588456
USP1 protein, partialHomo sapiens (human)Potency3.35870.031637.5844354.8130AID504865
NFKB1 protein, partialHomo sapiens (human)Potency5.62340.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency7.07950.35487.935539.8107AID624146
TDP1 proteinHomo sapiens (human)Potency15.06240.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency14.12540.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency19.62210.011212.4002100.0000AID1030
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.58930.00137.762544.6684AID914; AID915
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency18.83360.001530.607315,848.9004AID1224821
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.54810.035520.977089.1251AID504332
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency8.91251.000012.232631.6228AID1452
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency30.30010.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency0.00530.006026.168889.1251AID488953
mitogen-activated protein kinase 1Homo sapiens (human)Potency15.84890.039816.784239.8107AID995
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency28.18380.010323.856763.0957AID2662
gemininHomo sapiens (human)Potency26.91880.004611.374133.4983AID463097; AID504364
survival motor neuron protein isoform dHomo sapiens (human)Potency22.38720.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency10.00000.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency44.66840.177824.735279.4328AID488949
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency23.71500.058010.694926.6086AID588379
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.03550.00106.000935.4813AID943
lethal factor (plasmid)Bacillus anthracis str. A2012Potency7.94330.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency21.33130.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID459737Inhibition of soluble guanylyl cyclase in rat aortic smooth muscle cells assessed as inhibition of SNP-stimulated cGMP formation by immunoassay2010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Synthesis and biological evaluation of oxadiazole derivatives as inhibitors of soluble guanylyl cyclase.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID513573Induction of S-nitrosylation of TRPC5 in HEK cells assessed as increase in Ca2+ level from extracellular space at 10 uM2006Nature chemical biology, Nov, Volume: 2, Issue:11
Nitric oxide activates TRP channels by cysteine S-nitrosylation.
AID459739Inhibition of soluble guanylyl cyclase in rat aortic smooth muscle cells assessed as inhibition of SNP-stimulated cGMP formation at 10 uM by immunoassay2010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Synthesis and biological evaluation of oxadiazole derivatives as inhibitors of soluble guanylyl cyclase.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID459738Inhibition of soluble guanylyl cyclase in rat aortic smooth muscle cells assessed as inhibition of SNP-stimulated cGMP formation at 0.1 uM by immunoassay2010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Synthesis and biological evaluation of oxadiazole derivatives as inhibitors of soluble guanylyl cyclase.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (772)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's135 (17.49)18.2507
2000's496 (64.25)29.6817
2010's130 (16.84)24.3611
2020's11 (1.42)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 15.48

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index15.48 (24.57)
Research Supply Index6.68 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (15.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (0.38%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other790 (99.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]